A Designer Bleomycin with Significantly Improved DNA Cleavage Activity
نویسندگان
چکیده
منابع مشابه
A designer bleomycin with significantly improved DNA cleavage activity.
The bleomycins (BLMs) are used clinically in combination with a number of other agents for the treatment of several types of tumors, and the BLM, etoposide, and cisplatin treatment regimen cures 90-95% of metastatic testicular cancer patients. BLM-induced pneumonitis is the most feared, dose-limiting side effect of BLM in chemotherapy, which can progress into lung fibrosis and affect up to 46% ...
متن کاملBleomycin congeners exhibiting altered DNA cleavage specificity.
Sir: The bleomycins (BLM’s) are a family of structurally complex glycoprotein antibiotics possessing significant anticancer activity ( I ) . They have been demonstrated to effect DNA strand scission in a reaction that is both metal ion and oxygen dependent (2); this transformation is believed to form the basis for the therapeutic efficacy of the bleomycins. A number of studies have demonstrated...
متن کاملMechanism of double-strand DNA cleavage effected by iron-bleomycin.
We have observed that in the absence of hydrogen peroxide the Fe(III)-bleomycin (BLM) complex exhibits high DNA cleavage efficiency, converting supercoiled Form I DNA (pBR322 or phix174) to Form II (nicked, relaxed circular); the present study may give an important clue to elucidate the fact that iron-bleomycin mediated double-strand DNA cleavage requires at least one molecule of oxygen (O2) ov...
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We investigated the amplification of bleomycin-induced DNA cleavage by synthetic pyrrole triamide (PyPyPy) using 32P-labeled DNA fragments obtained from human genes. Peplomycin, a kind of bleomycins, plus Fe(II) caused DNA cleavage at the 5'-GC-3' and 5'-GT-3' sequences (damaged bases are underlined). The addition of PyPyPy enhanced the cleavage at cytosine and thymine residues 3' to consecutiv...
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In a recent study, we described the enhanced double-strand cleavage of hairpin DNAs by Fe·bleomycin (Fe·BLM) that accompanies increasingly strong binding of this antitumor agent and suggested that this effect may be relevant to the mechanism by which BLM mediates its antitumor effects. Because the DNA in tumor cells is known to be hypomethylated on cytidine relative to that in normal cells, it ...
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ژورنال
عنوان ژورنال: Journal of the American Chemical Society
سال: 2012
ISSN: 0002-7863,1520-5126
DOI: 10.1021/ja3056535